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Description
Application Note: G-1 is a potent and selective G protein-coupled estrogen receptor (GPER) agonist (Ki = 11 nM, EC50 = 2 nM), displays no activity at ERalpha and ERbeta at concentrations up to 10 ?M. Increases cytosolic Ca2+ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants (IC50 values are 0.7 and 1.6 nM respectively) in vitro. Blocks MCF-1 cell cycle progression at the G1 phase. Displays therapeutic effects in the mouse EAE model of multiple sclerosis.
Structure formula

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